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A2AAR antagonist 4 is an orally active antagonist of the A2A adenosine receptor (A2AAR) with a Ki value of 0.36 nM and a KB value of 1 nM in humans. At a concentration of 10 μM, it fully inhibits both human A2AAR and human A2bAR. A2AAR antagonist 4 is applicable in cancer research, such as studies involving MC38 tumors.
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| Description | A2AAR antagonist 4 is an orally active antagonist of the A2A adenosine receptor (A2AAR) with a Ki value of 0.36 nM and a KB value of 1 nM in humans. At a concentration of 10 μM, it fully inhibits both human A2AAR and human A2bAR. A2AAR antagonist 4 is applicable in cancer research, such as studies involving MC38 tumors. |
| Targets&IC50 | A2B (human):85.8 nM (Ki) |
| In vitro | A2AAR antagonist 4 (Compound 4d) at a concentration of 10 μM completely inhibits hA2A AR, hA2B AR, and hA3 AR in the CHO-A2A cell line. Additionally, A2AAR antagonist 4, within the range of 0.1-1000 nM, restores IL-2 secretion in PBMC cells by fully displacing NECA, with an EC50 value of 2.06 nM. |
| In vivo | Compound 4d, an A2AAR antagonist, significantly inhibits tumor growth in MC38 tumor-bearing mice when administered at 100 mg/kg orally or 50 mg/kg via intraperitoneal injection, twice daily for 14 days. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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